Classifications

• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K31/00—Medicinal preparations containing organic active ingredients
  • A61K31/60—Salicylic acid; Derivatives thereof
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K8/00—Cosmetics or similar toiletry preparations
  • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
  • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
  • A61K8/33—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
  • A61K8/36—Carboxylic acids; Salts or anhydrides thereof
  • A61K8/365—Hydroxycarboxylic acids; Ketocarboxylic acids
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K8/00—Cosmetics or similar toiletry preparations
  • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
  • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
  • A61K8/33—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
  • A61K8/36—Carboxylic acids; Salts or anhydrides thereof
  • A61K8/368—Carboxylic acids; Salts or anhydrides thereof with carboxyl groups directly bound to carbon atoms of aromatic rings
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P17/00—Drugs for dermatological disorders
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
  • A61Q19/00—Preparations for care of the skin

Definitions

• the present invention relates to compositions for topical anti-acne treatment. More particularly, the invention comprises salicylic acid and lactic acid adjusted to a selected pH and combined with a suitable vehicle for treating adult acne and sensitive skin conditions such as rosacea complicated with acne.
• Rosacea complicated with acne is difficult to treat because of the tendency for hypersensitivity and side effects in this group, particularly when known alcoholic solutions, lotions and gels are applied to an individual's skin.
• Irritant folliculiti ⁇ caused by epithelial irritations, is another sensitive skin condition which manifests as erythematous papules and follicular pustules. Recurrent episodes of irritant folliculitis are sometimes misdiagnosed as common acne and treated with physical abrasives and exfoliants which traumatize and aggravate the original condition.
• U.S. Patent No. 4,800,197 describes a combination of salicylic acid and an anionic taurate surfactant, specifically sodium methyl cocoyl taurate or sodium methyl oleoyl taurate.
• U.S. Patent No. 5,296,476 describes the specific use of salicylic acid in combination with calcium citrate. Again, these treatment modalities are designed 4 for aggressive, physical cleansing, which assumes that the individual indicators are normal, young and oily skin.
• salicylic acid tend to aggravate the relatively dry adult acne, and they are particularly unsuitable for those with sensitive skin conditions such as irritant folliculitis.
• Known salicylic acid preparations are also poorly tolerated in patients suffering from acne complexed with rosacea.
• lactic acid for teenage problem skin. See, for example, U.S. Patent Nos. 3,879,537, 4,234,599, 4,363,815 and 4,380,549 which generally describe the use of alpha-hydroxy acids such as lactic and citric acids for titrating pH in antibiotic preparations. These antibiotic therapies assume that teen acne has predominant etiological ties to opportunistic bacterial infections like those found in acne vulgaris.
• U.S. Patent No. 4,507,319 describes the use of lactic acid for adjusting pH in a composition comprising derivatives of 2-hydroxy-octanoic acid or 2-keto-octanoic acid; and
• U.S. Patent No. 4,330,531 describes a germ killing composition containing lactic acid which produces chlorine dioxide gas for antibacterial effects on acne vulgaris.
• U.S. Patent No. 3,806,593 discloses the use of esters of lactic acid; and U.S. Patent No. 4,540,567 describes the use of lactate esters, preferably ethyl lactate.
• U.S. Patent Nos. 4,613,592 and 4,772,592 also refer to lactate esters in compositions which have silicone oil and a ⁇ -C ⁇ alkanol.
• a further object of the present invention is to provide a composition containing a selected range of lactic acid which has a synergistic effect with a selected range of salicylic acid for raising the tolerance levels of sensitive skin to both ingredients, while providing the therapeutic benefits of the two ingredients.
• the present invention is directed to a mild, topical formulation for treating adult acne and sensitive skin conditions complicated with acne, which comprises about 0.05 to about 5.0% salicylic acid; about 0.5 to about 15.0% lactic acid; sufficient pH adjustor to maintain pH in the range of about 3.8 to about 4.5; and a vehicle which maintains the active ingredient levels, desired pH and mildness.
• a lotion embodiment may have about 6.5% propylene glycol dicaprylate/dicaprate; about 6.0% lactic acid; about 5.0% glycerin; about 3.0% ammonium hydroxide; about 2.0% Peg 40 Stearate; about 1.5% Steareth-2; about 0.6% hydroxyethyl cellulose; about 0.6% xanthan gum; about 0.5% salicylic acid; about 0.2% methylparaben; about 0.2% disodium EDTA; about 0.2% vitamin-E acetate and about 0.3% natural extracts from apple, grape, mango, orange and geranium.
• One inventive composition includes salicylic acid and lactic acid adjusted to selected pH ranges and mixed in a suitable vehicle such as lotions, creams, gels or other carriers which maintain the active ingredient levels, desired pH and inherent mildness.
• a suitable vehicle such as lotions, creams, gels or other carriers which maintain the active ingredient levels, desired pH and inherent mildness.
• the general and preferred ranges in the following examples are expressed as weight percents.
• Salicylic Acid 0.05-5.0% 0.5-2.0%
• Lactic Acid 0.5-15.0% 5.0-10.0% Glycerin 0.1-10.0% 0.5-6.0%
• Peg 40 Stearate 0.5-5.0% 1.8-4.0%
• Methylparaben 0.1-0.3% 0.20-0.25%
• glycerin acts as a humectant and moisturizer
• propylene glycol dicaprylate/ dicaprate is used as an emollient/moistur ⁇ izer
• Peg-40 stearate and Steareth-2 act as the primary and secondary emulsifiers, respectively
• xanthan gum and hydroxyethyl cellulose are used for thickening
• disodium EDTA acts as a chelator to sequester any discoloration causing metal ions
• methylparaben is used as a preservative.
• Ammonium hydroxide is used to partially neutralize the lactic and salicylic acids and raise the pH to its required levels.
• Other suitable pH adjustors include sodium hydroxide, potassium hydroxide and triethanolamine.
• Salicylic Acid 0.05-5.0% 0.5-2.0% Lactic Acid 0.5-15.0% 5.0-10.0% Glycerin 0.1-5.0% 0.5-4.0%
• Vitamin E Acetate 0.05-0.2% 0.1-0.2%
• glycerin, propylene glycol dicaprylate/dicaprate, disodium EDTA and ammonium hydroxide perform similar functions described for the lotion embodiment.
• Steareth-20 and Steareth-2 act as the primary and secondary emulsifiers, respectively; cetyl alcohol, glyceryl monostearate, xanthan gum and hydroxy ⁇ ethyl cellulose are all used for thickening; and imidazol ⁇ idinyl urea is used as a preservative.
• Salicylic Acid 0.05-4.0% 0.5-2.0% Lactic Acid 0.5-12.0% 4.0-9.0% Disodium EDTA 0.05-0.25% 0.15-0.20% Propylene Glycol 0.5-9.0% 2.0-6.0% Hydroxyethyl Cellulose 0.3-2.0% 0.4-1.5% Botanical Extracts 0.1-2.0% 0.2-1.5% Methylparaben 0.1-0.3% 0.20-0.25%
• disodium EDTA, hydroxyethyl cellulose, methylparaben and ammonium hydroxide perform the same or similar functions disclosed for the lotion and cream embodiments.
• Propylene glycol acts as a humectant and botanical extracts (such as chamomile extract) contributes to gentleness.
• Glycerin was next added (for lotion and cream embodiments) and mixed continuously for 10-15 minutes. Hydroxyethylcellulose and other thickeners were then slowly sprinkled into the mixture and the sweep was disengaged. The resulting batch was milled (an equivalent vigorous high shear type of mixing is equally effective) for about one hour until a uniform consistency was achieved. Sweep mixing was then resumed and any entrapped air was allowed to rise in this first phase. The temperature was maintained in the first tank at about 160- 165°F.
• the oil phase plus emulsifiers were heated at 170-175°F and mixed to a uniform consistency.
• the ingredients in this step were propylene glycol dicaprylate/dicaprate, methylparaben, Steareth-2 and Peg 40 stearate; in the cream, the ingredients comprised propylene glycol dicaprylate/ dicaprate, Steareth-20 and Steareth-2; and in the gel, the ingredients included propylene glycol and methylparaben.
• the resulting mixture in the second tank) was put through a 200 micron strainer and subsequently added to the first tank containing the first phase.
• the first phase (in the first tank) was continuously milled during transfer and the resulting batch was further milled for about five minutes after the transfer operation was complete. Following milling, the batch was sweep- mixed slowly for about 10 minutes and allowed to cool to 90-95°F. Slow mixing was continued and other ingredients such as vitamins, botanicals, additional emollients and oils, to suit the particular target product variations, were added. Fragrances were next added.
• additional ingredients can be introduced in this concluding step or earlier to create other variations which are covered by the scope of this disclosure.
• the study design included an eight week facial use test, with periodic telephone callback interviews. This quantitative study was fielded in five geographically dispersed locations, for a total of 200 women, with 40 per location. All raw data was processed through statistical analysis using the SAS statistical package.
• the study was a baseline controlled six month test, with evaluations of facial skin occurring at 4, 9, 12, 18 and 24 weeks.
• the product's effectiveness was principally evaluated by clinical grades from attending dermatolog ⁇ ists. Panelists returned to the study site every two weeks for a compliance check.
• Fitzpatrick scale Skin Types I, II or III. A recent history of acne breakout or similar skin disorders was also required. Each participant was examined by a physician to confirm the existence of one or more of the following conditions.
• Follicular papules small pin-point sized raised bumps associated with irritation of the follicles 2.
• Papules relatively large red inflammatory lesions
• Blackheads - a specific type of clogged pore which is covered with a black "cap” and is slightly raised above the skin surface
• rosacea attributes were recorded by noting diffuse redness and general erythema of the skin caused by permanently dilated capillaries or telangiectasia.
• the test product was a white lotion with a light citrus scent. It contained 0.5% salicylic acid and 6.0% lactic acid, with a pH between 4.2 and 4.4.
• the lotion was supplied in four 1 ounce glass bottles. For the first two weeks, test participants were instructed to apply the lotion once a day, preferably at night after cleansing the face. After two weeks, the lotion was applied in the morning and evening until symptoms were diminished.
• Test results were collected in response to written and oral questions. Statistical analysis of the raw data was performed by a consulting statistician. Incomplete data was excluded from the analysis and conventional methods were used to verify statistical significance.

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• 1996
  • 1996-02-20 JP JP8526992A patent/JPH09511769A/ja active Pending
  • 1996-02-20 WO PCT/US1996/002938 patent/WO1996027365A1/en not_active Application Discontinuation
  • 1996-02-20 CA CA002187917A patent/CA2187917A1/en not_active Abandoned
  • 1996-02-20 EP EP96909570A patent/EP0756479A4/de not_active Withdrawn
  • 1996-02-20 AU AU53018/96A patent/AU5301896A/en not_active Abandoned

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